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Abstract PR006: Target validation and drug discovery efforts on exoribonuclease XRN1

Maureen M. Lynes, Gordon J. Lockbaum, Brian A. Sparling, Sophie A. Shen, Sunaina P. Nayak, Kevin Knockenhauer, Simina Grigoriu, Shane M. Buker, Kenneth W. Duncan, Robert A. Copeland, Stephen J. Blakemore, Serena J. Silver, P. Ann Boriack-Sjodin

Mol Cancer Ther (2024) 23 (11_Supplement): PR006.

https://doi.org/10.1158/1538-8514.RNADRIVERS24-PR006

Published: 14 November 2024

View articletitled, Abstract PR006: Target validation and drug discovery efforts on exoribonuclease XRN1

Journal Articles

Abstract PR001: KIF18A inhibition, via ATX020, leads to mitotic arrest and robust anti-tumor activity through a synthetic lethal interaction with chromosome instability

Maureen S. Lynes, Laura Ghisolfi, Sanjoy Khan, Taylor Hotz, Brian A. Sparling, Mary-Margaret Zablocki, Deepali Gotur, P. Ann Boriack-Sjodin, Kenneth W. Duncan, Stephen J. Blakemore, Serena J. Silver, Robert A. Copeland

Mol Cancer Ther (2024) 23 (6_Supplement): PR001.

https://doi.org/10.1158/1538-8514.SYNTHLETH24-PR001

Published: 10 June 2024

View articletitled, Abstract PR001: KIF18A inhibition, via ATX020, leads to mitotic arrest and robust anti-tumor activity through a synthetic lethal interaction with chromosome instability

Journal Articles

Abstract A001: KIF18A inhibition, via ATX020, leads to mitotic arrest and robust anti-tumor activity through a synthetic lethal interaction with chromosome instability

Maureen S. Lynes*, Laura Ghisolfi†, Sanjoy Khan, Taylor Hotz, Brian A. Sparling, Mary-Margaret Zablocki, Deepali Gotur, P. Ann Boriack-Sjodin, Kenneth W. Duncan, Stephen J. Blakemore, Serena J. Silver, Robert A Copeland

Mol Cancer Ther (2024) 23 (6_Supplement): A001.

https://doi.org/10.1158/1538-8514.SYNTHLETH24-A001

Published: 10 June 2024

View articletitled, Abstract A001: KIF18A inhibition, via ATX020, leads to mitotic arrest and robust anti-tumor activity through a synthetic lethal interaction with chromosome instability

Journal Articles

Abstract IA024: RNA-modifying enzyme inhibitors as synthetic lethal cancer therapeutics

Mol Cancer Ther (2024) 23 (6_Supplement): IA024.

https://doi.org/10.1158/1538-8514.SYNTHLETH24-IA024

Published: 10 June 2024

View articletitled, Abstract IA024: RNA-modifying enzyme inhibitors as synthetic lethal cancer therapeutics

Journal Articles

Abstract A170: Discovery of small molecule inhibitors of ADAR1

Shane M Buker, Stephen J Blakemore, P. Ann Boriack-Sjodin, Cindy Collins, Robert A Copeland, Kenneth W Duncan, Anna Ericsson, Alexandra Garadino, April Greene-Colozzi, Nathalie Leger, Gordon Lockbaum, Anugraha Raman, Scott Ribich, Allen Sickmier, Brian S Sparling, Jie Wu, Serena Silver

Mol Cancer Ther (2023) 22 (12_Supplement): A170.

https://doi.org/10.1158/1535-7163.TARG-23-A170

Published: 01 December 2023

View articletitled, Abstract A170: Discovery of small molecule inhibitors of ADAR1

Journal Articles

Abstract B073: Characterization of selective, allosteric inhibitors of human XRN1

Gordon J Lockbaum, E. Allen Sickmier, Brian A Sparling, Kevin Knockenhauer, Nicholas Holt, Julie Liu, Maureen M Lynes, Simina Grigoriu, Kenneth W Duncan, Robert A Copeland, P. Ann Boriack-Sjodin

Mol Cancer Ther (2023) 22 (12_Supplement): B073.

https://doi.org/10.1158/1535-7163.TARG-23-B073

Published: 01 December 2023

View articletitled, Abstract B073: Characterization of selective, allosteric inhibitors of human XRN1

Journal Articles

Abstract C087: DHX9 inhibition as a novel therapeutic modality in microsatellite instable colorectal cancer

Mol Cancer Ther (2023) 22 (12_Supplement): C087.

https://doi.org/10.1158/1535-7163.TARG-23-C087

Published: 01 December 2023

View articletitled, Abstract C087: DHX9 inhibition as a novel therapeutic modality in microsatellite instable colorectal cancer

Journal Articles

Abstract B130: Elevated cancer-intrinsic type I interferon signaling confers a dependency on the RNA editor ADAR1

Alexandra K. Gardino, Cindy Collins, Maureen S. Lynes, P. Ann Boriack-Sjodin, Robert A. Copeland, Scott A. Ribich

Mol Cancer Ther (2019) 18 (12_Supplement): B130.

https://doi.org/10.1158/1535-7163.TARG-19-B130

Published: 01 December 2019

View articletitled, Abstract B130: Elevated cancer-intrinsic type I interferon signaling confers a dependency on the RNA editor ADAR1

Journal Articles

Abstract A112: Drug discovery efforts on the RNA protein methyltransferase METTL3/METTL14

P. Ann Boriack-Sjodin, Alexandra K. Gardino, Thomas A. Wynn, Shane M. Buker, Monique Laidlaw, E. Allen Sickmier, Brian L. Hodous, April W. Case, April E. Greene-Colozzi, Robert A. Copeland, Scott Ribich

Mol Cancer Ther (2019) 18 (12_Supplement): A112.

https://doi.org/10.1158/1535-7163.TARG-19-A112

Published: 01 December 2019

View articletitled, Abstract A112: Drug discovery efforts on the RNA protein methyltransferase METTL3/METTL14

Journal Articles

EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL

Dorothy Brach, Danielle Johnston-Blackwell, Allison Drew, Trupti Lingaraj, Vinny Motwani, Natalie M. Warholic, Igor Feldman, Christopher Plescia, Jesse J. Smith, Robert A. Copeland, Heike Keilhack, Elayne Chan-Penebre, Sarah K. Knutson, Scott A. Ribich, Alejandra Raimondi, Michael J. Thomenius

Mol Cancer Ther (2017) 16 (11): 2586–2597.

https://doi.org/10.1158/1535-7163.MCT-16-0840

Published: 01 November 2017

View articletitled, EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL

Includes: Supplementary data

Journal Articles

Mechanisms of Pinometostat (EPZ-5676) Treatment–Emergent Resistance in MLL-Rearranged Leukemia

Carly T. Campbell, Jessica N. Haladyna, David A. Drubin, Ty M. Thomson, Michael J. Maria, Taylor Yamauchi, Nigel J. Waters, Edward J. Olhava, Roy M. Pollock, Jesse J. Smith, Robert A. Copeland, Stephen J. Blakemore, Kathrin M. Bernt, Scott R. Daigle

Mol Cancer Ther (2017) 16 (8): 1669–1679.

https://doi.org/10.1158/1535-7163.MCT-16-0693

Published: 02 August 2017

View articletitled, Mechanisms of Pinometostat (EPZ-5676) Treatment–Emergent Resistance in MLL-Rearranged Leukemia

Includes: Supplementary data

Journal Articles

Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models

Elayne Chan-Penebre, Kelli Armstrong, Allison Drew, Alexandra R. Grassian, Igor Feldman, Sarah K. Knutson, Kristy Kuplast-Barr, Maria Roche, John Campbell, Peter Ho, Robert A. Copeland, Richard Chesworth, Jesse J. Smith, Heike Keilhack, Scott A. Ribich

Mol Cancer Ther (2017) 16 (5): 850–860.

https://doi.org/10.1158/1535-7163.MCT-16-0678

Published: 02 May 2017

View articletitled, Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models

Includes: Supplementary data

Journal Articles

Abstract B78: CRISPR pooled screening identifies differential dependencies on epigenetic pathways

Alexandra R. Grassian, Julian Fowler, Igor Feldman, Thomas Riera, Darren Harvey, Allison E. Drew, Richard Chesworth, Robert A. Copeland, Heike Keilhack, Jesse J. Smith, Scott Ribich

Mol Cancer Ther (2015) 14 (12_Supplement_2): B78.

https://doi.org/10.1158/1535-7163.TARG-15-B78

Published: 01 December 2015

View articletitled, Abstract B78: CRISPR pooled screening identifies differential dependencies on epigenetic pathways

Journal Articles

Abstract C87: EZH2 inhibition leads to decreased proliferation in SMARCA4-deleted ovarian cancer cell lines

Sarah K. Knutson, Allison E. Drew, Christopher Plescia, Robert A. Copeland, Jesse J. Smith, Heike Keilhack, Scott Ribich

Mol Cancer Ther (2015) 14 (12_Supplement_2): C87.

https://doi.org/10.1158/1535-7163.TARG-15-C87

Published: 01 December 2015

View articletitled, Abstract C87: EZH2 inhibition leads to decreased proliferation in SMARCA4-deleted ovarian cancer cell lines

Journal Articles

Abstract C85: Identification of a novel potent selective SMYD3 inhibitor with oral bioavailability

Mol Cancer Ther (2015) 14 (12_Supplement_2): C85.

https://doi.org/10.1158/1535-7163.TARG-15-C85

Published: 01 December 2015

View articletitled, Abstract C85: Identification of a novel potent selective SMYD3 inhibitor with oral bioavailability

Journal Articles

Abstract A135: Physiologically-based pharmacokinetic modeling to support clinical investigation of the EZH2 inhibitor, tazemetostat (EPZ-6438) in INI1-deficient pediatric tumors

Nathalie Rioux, Heike Keilhack, Blythe Thomson, Richard Chesworth, Robert A. Copeland, Eric Hedrick, Peter Ho, Nigel J. Waters

Mol Cancer Ther (2015) 14 (12_Supplement_2): A135.

https://doi.org/10.1158/1535-7163.TARG-15-A135

Published: 01 December 2015

View articletitled, Abstract A135: Physiologically-based pharmacokinetic modeling to support clinical investigation of the EZH2 inhibitor, tazemetostat (EPZ-6438) in INI1-deficient pediatric tumors

Journal Articles

Abstract B85: EZH2 plays a critical role in B-cell maturation and in non-Hodgkin's lymphoma: Interplay between EZH2 function and B-cell activation

Danielle Johnston, Dorothy Brach, Christopher Plescia, Alison Drew, Trupti Lingaraj, Natalie Warholic, Jesse J. Smith, Robert A. Copeland, Heike Keilhack, Elayne Penebre, Sarah K. Knutson, Scott Ribich, Michael J. Thomenius, Alejandra Raimondi

Mol Cancer Ther (2015) 14 (12_Supplement_2): B85.

https://doi.org/10.1158/1535-7163.TARG-15-B85

Published: 01 December 2015

View articletitled, Abstract B85: EZH2 plays a critical role in B-cell maturation and in non-Hodgkin's lymphoma: Interplay between EZH2 function and B-cell activation

Journal Articles

Abstract B82: Pinometostat (EPZ-5676) enhances the antiproliferative activity of MAP kinase pathway inhibitors in MLL-rearranged leukemia cell lines

Alejandra Raimondi, Christine R. Klaus, Jeffrey A. Keats, Scott R. Daigle, Robert A. Copeland, Jorge DiMartino, Jesse J. Smith, Stephen J. Blakemore

Mol Cancer Ther (2015) 14 (12_Supplement_2): B82.

https://doi.org/10.1158/1535-7163.TARG-15-B82

Published: 01 December 2015

View articletitled, Abstract B82: Pinometostat (EPZ-5676) enhances the antiproliferative activity of MAP kinase pathway inhibitors in MLL-rearranged leukemia cell lines

Journal Articles

Abstract C162: A medium-throughput single cell CRISPR-Cas9 assay to assess gene essentiality

Alexandra R. Grassian, Tim Scales, Sarah K. Knutson, Nicola J. McCarthy, Chris E. Lowe, Jon D. Moore, Robert A. Copeland, Heike Keilhack, Jesse J. Smith, Julie A. Wickendon, Scott Ribich

Mol Cancer Ther (2015) 14 (12_Supplement_2): C162.

https://doi.org/10.1158/1535-7163.TARG-15-C162

Published: 01 December 2015

View articletitled, Abstract C162: A medium-throughput single cell CRISPR-Cas9 assay to assess gene essentiality

Journal Articles

Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma

Mol Cancer Ther (2014) 13 (4): 842–854.

https://doi.org/10.1158/1535-7163.MCT-13-0773

Published: 06 April 2014

View articletitled, Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma

Includes: Supplementary data

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Abstract PR006: Target validation and drug discovery efforts on exoribonuclease XRN1

Abstract PR001: KIF18A inhibition, via ATX020, leads to mitotic arrest and robust anti-tumor activity through a synthetic lethal interaction with chromosome instability

Abstract A001: KIF18A inhibition, via ATX020, leads to mitotic arrest and robust anti-tumor activity through a synthetic lethal interaction with chromosome instability

Abstract IA024: RNA-modifying enzyme inhibitors as synthetic lethal cancer therapeutics

Abstract A170: Discovery of small molecule inhibitors of ADAR1

Abstract B073: Characterization of selective, allosteric inhibitors of human XRN1

Abstract C087: DHX9 inhibition as a novel therapeutic modality in microsatellite instable colorectal cancer

Abstract B130: Elevated cancer-intrinsic type I interferon signaling confers a dependency on the RNA editor ADAR1

Abstract A112: Drug discovery efforts on the RNA protein methyltransferase METTL3/METTL14

EZH2 Inhibition by Tazemetostat Results in Altered Dependency on B-cell Activation Signaling in DLBCL

Mechanisms of Pinometostat (EPZ-5676) Treatment–Emergent Resistance in MLL-Rearranged Leukemia

Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models

Abstract B78: CRISPR pooled screening identifies differential dependencies on epigenetic pathways

Abstract C87: EZH2 inhibition leads to decreased proliferation in SMARCA4-deleted ovarian cancer cell lines

Abstract C85: Identification of a novel potent selective SMYD3 inhibitor with oral bioavailability

Abstract A135: Physiologically-based pharmacokinetic modeling to support clinical investigation of the EZH2 inhibitor, tazemetostat (EPZ-6438) in INI1-deficient pediatric tumors

Abstract B85: EZH2 plays a critical role in B-cell maturation and in non-Hodgkin's lymphoma: Interplay between EZH2 function and B-cell activation

Abstract B82: Pinometostat (EPZ-5676) enhances the antiproliferative activity of MAP kinase pathway inhibitors in MLL-rearranged leukemia cell lines

Abstract C162: A medium-throughput single cell CRISPR-Cas9 assay to assess gene essentiality

Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma

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